Substitution of a triazole for the central olefin in biologically active stilbenes.
Basic Information
ID: ALA5236570
Journal: Bioorg Med Chem Lett
Title: Substitution of a triazole for the central olefin in biologically active stilbenes.
Authors: Stockdale DP, Beutler JA, Wiemer DF.
Abstract: The stilbene moiety is commonly found in natural products and these compounds display an extraordinary range of biological activity. Efforts to derive useful drugs from stilbenes must address the potential liabilities of this structure, including a propensity for cis/trans isomerization. To identify olefin replacements that address this limitation while preserving biological activity we have prepared analogues of two bioactive stilbenes, a pawhuskin and a schweinfurthin, where a 1,2,3-triazole ring formally replaces the stilbene double bond. The new schweinfurthin analogue (23) has been tested for anti-proliferative activity against 60 cell lines, and shows a strong correlation of bioactivity when compared to the compound that inspired its synthesis (22).
CiteXplore: 36096344
DOI: 10.1016/j.bmcl.2022.128980
Patent ID: ┄